Development and Evaluation of Sildenafil Citrate Tablet Fabricated by Direct Compression Method

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Chiravut Pathumthanasup
Kutcharin Phunikhom
Jomjai Peerapattana

Abstract

The objective of this research was to develop the formulas of sildenafil citrate tablet, normally used to treat erectile dysfunction diseases. The tablets were prepared by direct compression method. Each tablet consisted of the sildenafil citrate (equivalence to 10 mg of sildenafil), direct compression excipients as spray dried lactose (SDL) or microcrystalline cellulose (MCC) or combination of SDL with MCC in a ratio of 1: 1, glidants as 0.2% of colloidal silicon dioxide and lubricants as 1% of magnesium stearate. These formulations were evaluated for powder properties. Each formulations were compressed to crushing strength (CS) at 4 and 8 kgf at 100 mg per tablet. These tablets were evaluated for tablet quality. The results showed that the formulation contained SDL had excellent powder flow properties. The formulation contained SDL: MCC (1: 1) had powder flow properties better than that using only MCC. Each formulation met the acceptance criteria of weight variation and uniformity of dosage units in the pharmacopoeia. The tablets used MCC had low friability (F) and disintegration time (DT). The tablets used combination of SDL: MCC (1: 1) exhibited lower F and DT than those using only SDL. These tablets, compressed to CS 8 kgf appeared higher crushing strength/friability ratio (CSFR) than those of 4 kgf tablets, whereas a CSFR/DT was lower than that of 4 kgf tablets. Drug Release of sildenafil citrate from tablets used MCC and SDL: MCC (1: 1) at CS 4 and 8 kgf at 15 min were greater than 80% and met the standard requirement of dissolution test in the pharmacopoeia. It can be concluded that direct compressed tablet of sildenafil citrate consisting of the MCC or SDL: MCC (1: 1), colloidal silicon dioxide, and magnesium stearate, and then compressed to CS 4 and 8 kgf are complied with the United States Pharmacopeia (USP 40/NF 35) and might be used as guidance for development of low-dose formulation of tablets for safe treatment and reducing side effects from high-dose tablet.

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Pharmaceutical Sciences

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